One‐Pot Synthesis of 8‐Azaguanines by Transition Metal‐Free Cascade Cyclization of Carbodiimides with Ethyl Diazoacetate

Abstract A concise and mild method to construct 8‐azaguanines derivatives in one‐pot fashion has been developed. This strategy involves a rapid assembly of ethyl diazoacetate (EDA) with two carbodiimides via a cascade cyclization process. A variety of diversely substituted 8‐azaguanines derivatives were prepared with good regioselectivity and yields. The facile scale‐up synthesis further revealed the promising utility of this methodology.